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Class: Dihydropyridines
- Calcium-Channel Blocking Agents, Dihydropyridine
- Calcium Antagonists
VA Class: CV200
Chemical Name: 4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester
Molecular Formula: C19H21N3O5
CAS Number: 75695-93-1

Medically reviewed by Last updated on Jan 28, 2019.


Calcium-channel blocking agent; dihydropyridine derivative.1 2 3 4 7

Uses for Isradipine


Management of hypertension (alone or in combination with other classes of antihypertensive agents).1 2 3 4 6 7 13 14 15 500

Calcium-channel blockers are recommended as one of several preferred agents for the initial management of hypertension; other options include ACE inhibitors, angiotensin II receptor antagonists, and thiazide diuretics.501 502 503 504 While there may be individual differences with respect to specific outcomes, these antihypertensive drug classes all produce comparable effects on overall mortality and cardiovascular, cerebrovascular, and renal outcomes.500 501 502 504 Individualize choice of therapy; consider patient characteristics (e.g., age, ethnicity/race, comorbidities, cardiovascular risk) as well as drug-related factors (e.g., ease of administration, availability, adverse effects, cost).500 501 502 503 504 515

Calcium-channel blockers may be preferred in hypertensive patients with certain coexisting conditions (e.g., ischemic heart disease)523 and in geriatric patients, including those with isolated systolic hypertension.502 510

Black hypertensive patients generally respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to other antihypertensive drug classes (e.g., ACE inhibitors, angiotensin II receptor antagonists).500 501 504 However, diminished response to these other drug classes is largely eliminated when administered concomitantly with a calcium-channel blocker or thiazide diuretic.500 504

The optimum BP threshold for initiating antihypertensive drug therapy is controversial.501 504 505 506 507 508 515 523 530 Further study needed to determine optimum BP thresholds/goals; individualize treatment decisions.501 503 507 515 526 530

JNC 7 recommends initiation of drug therapy in all patients with uncomplicated hypertension and BP ≥140/90 mm Hg;500 JNC 8 panel recommends SBP threshold of 150 mm Hg for patients ≥60 years of age.501 Although many experts agree that SBP goal of <150 mm Hg may be appropriate for patients ≥80 years of age,502 504 505 530 application of this goal to those ≥60 years of age is controversial, especially for those at higher cardiovascular risk.501 502 505 506 508 511 515

In the past, initial antihypertensive drug therapy was recommended for patients with diabetes mellitus or chronic kidney disease who had BP ≥130/80 mm Hg;500 503 current hypertension management guidelines generally recommend a BP threshold of 140/90 mm Hg for these individuals (same as for the general population of patients without these conditions), although a goal of <130/80 mm Hg may still be considered.501 502 503 504 520 530 535 536 541

Use of currently available conventional dosage form for acute management of hypertensive crises not established.4 50

Isradipine has been used for rapid reduction of BP in pediatric patients 1–17 years of age with severe hypertension.76 83

Isradipine Dosage and Administration


BP Monitoring and Treatment Goals

  • Carefully monitor BP during initial titration or subsequent upward adjustment in dosage.500 501

  • When available, use evidence-based dosing information (i.e., dosages shown in randomized controlled trials to reduce complications of hypertension) to determine target dosages; target dosages usually can be achieved within 2–4 weeks but may take up to several months.501

  • If adequate BP response not achieved with a single antihypertensive agent, add a second drug with demonstrated benefit; if goal BP still not achieved with optimal dosages of 2 antihypertensive agents, add a third drug.501 May maximize dosage of the first drug before adding a second drug, or add a second drug before maximizing dosage of the initial drug.501

  • Consider initiating antihypertensive therapy with a combination of drugs if patient's BP exceeds goal BP by >20/10 mm Hg.500 501 503 504

  • Goal is to achieve and maintain optimal control of BP; individualize specific target BP based on consideration of multiple factors, including patient age and comorbidities, and currently available evidence from clinical studies.500 501 (See Hypertension under Uses.)


Oral Administration

Conventional Capsules

Administer orally twice daily without regard to meals.1 22


Preparation of extemporaneous suspension containing isradipine 1 mg/mL: Open twenty-four 5-mg capsules and grind contents to a fine powder with a mortar and pestle;76 levigate with a small amount of glycerin to form a paste.81 Add simple syrup in increasing amounts while mixing thoroughly; transfer suspension to a graduated cylinder.81 Add any remaining drug in the mortar to the graduated container; the final volume of the suspension should be 120 mL.81 Transfer suspension to an amber bottle.81 Shake well before each use.81


Pediatric Patients


Initially, 0.15–0.2 mg/kg daily given in 3–4 divided doses.76 Increase dosage as necessary up to a maximum dosage of 0.8 mg/kg (up to 20 mg) daily.76

Severe Hypertension
Rapid Reduction of BP

Children and adolescents 1–17 years of age: 0.05–0.1 mg/kg per dose.76



Initially, 1.25–2.5 mg twice daily 1 2 3 4 7 14 15 16 50 as monotherapy or when added to thiazide diuretic therapy.1

Full hypotensive effect may not be seen for 2–4 weeks.1 If BP control is inadequate after this period, increase dosage in increments of 5 mg daily at intervals of 2–4 weeks, up to a maximum of 20 mg daily, according to patient’s BP response.1 4 50 Some experts recommend usual dosage range of 2.5–10 mg daily.500

Dosages >10 mg daily usually do not result in further improvement in BP control and may increase risk of adverse effects.1 4 50

If intolerable adverse effects occur, consider dosage reduction; if adverse effects worsen or fail to resolve, may need to discontinue and switch to another antihypertensive drug class.501

Prescribing Limits

Pediatric Patients


Maximum 0.8 mg/kg (up to 20 mg) daily.76



Maximum 20 mg daily.1 4

Special Populations

Hepatic Impairment

Some clinicians recommend dosage modification (i.e., reduced dosage) and careful titration,3 21 but the manufacturer recommends usual initial adult dosage.1 4 7

Renal Impairment

Dosage modification not necessary.1 4 7

Geriatric Patients

Initial dosage modification not necessary,1 3 4 7 16 20 but slower dosage escalation recommended;3 20 BP may be adequately controlled with relatively low dosages and once-daily dosing.2 3 16

Cautions for Isradipine


  • Known hypersensitivity to isradipine or any ingredient in the formulation.1


General Precautions


Possible symptomatic hypotension.1 Carefully monitor BP, especially during therapy initiation or dosage increase.1

Heart Failure

May precipitate or worsen heart failure.1 16 18 Use with caution and titrate dosage carefully, especially in those receiving concomitant β-adrenergic blocking agents.1 16 18


Frequency, duration, and severity of angina may rarely increase during therapy.3 14 18

Specific Populations


Category C.1


Not known whether isradipine is distributed into milk; discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy remain to be fully established in children;1 22 however, some experts have recommended dosages for hypertension based on current limited clinical experience.76

Common Adverse Effects

Headache, dizziness, peripheral edema, palpitation, tachycardia, flushing, chest pain.1 2 3 4 10 11 13 14 15 16 17 18 19 20 21 22 23 24 25 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 51 52 53

Interactions for Isradipine

Appears to be metabolized by CYP3A4.1

Specific Drugs





Increased peak plasma concentrations and AUC of isradipine1

Monitor carefully; reduction of isradipine dosage may be required1


Pharmacokinetic interaction unlikely1


Possible severe hypotension during fentanyl anesthesia with concomitant use of a β- blocker and a calcium channel blocker1

Increase volume of circulating fluids if hypotension occurs1


Pharmacokinetic interaction unlikely1


Pharmacokinetic interaction unlikely1


Increased rate of absorption, AUC, and peak plasma concentrations of propranolol observed with single doses; no substantial effect on either drug under steady-state conditions1


Increased isradipine metabolism and clearance; reduction of isradipine concentrations to below detectable levels1

Isradipine concentrations and therapeutic effects will be markedly reduced or abolished with concomitant use1


Pharmacokinetic or pharmacodynamic interaction unlikely

Isradipine Pharmacokinetics



90–95% absorbed following oral administration, with peak plasma isradipine concentrations attained in about 1.5 hours.1

Bioavailability is approximately 15–24% due to first-pass metabolism.1


After a single dose, reduction in supine and standing BP occurs within 2–3 hours.1


Effects persist for >12 hours after administration.1


Food decreases time to peak plasma concentration by about 1 hour.1

Special Populations

In patients with hepatic impairment, peak plasma concentration and AUC are increased by 32 and 52%, respectively.1

In patients with mild renal impairment (Clcr 30–80 mL/min), AUC is increased by 45%; however, in patients with severe renal failure (Clcr <10 mL/min) who have been on hemodialysis, AUC is decreased by 20–50%.1

In geriatric patients, peak plasma concentration and AUC are increased by 13 and 40%, respectively.1



It is not known whether isradipine is distributed into milk.1

Plasma Protein Binding




Completely metabolized in the liver, apparently by CYP3A4, to inactive metabolites.1

Elimination Route

Excreted in urine (60–65%) and feces (25–30%).1


Biphasic; initial half-life is 1.5–2 hours and terminal elimination half-life is approximately 8 hours.1




Conventional Capsules

Tight, light-resistant containers at 20–25°C.82

Extemporaneous Suspension

Isradipine 1 mg/mL in simple syrup (see Reconstitution under Dosage and Administration): Stable for 35 days when refrigerated.81


  • Inhibits transmembrane influx of extracellular calcium ions across the membranes of myocardial cells and vascular smooth muscle cells, without changing serum calcium concentrations.1

  • Peripheral arterial vasodilator; acts directly on vascular smooth muscle causing reduction in peripheral vascular resistance (afterload) and BP.1

Advice to Patients

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name



Dosage Forms


Brand Names




2.5 mg*

Isradipine Capsules

5 mg*

Isradipine Capsules

AHFS DI Essentials™. © Copyright 2019, Selected Revisions January 26, 2015. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.


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